SALT OF MORPHOLINE DERIVATIVE AND CRYSTALLINE FORM THEREOF, AS WELL AS PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE OF THE SAME

The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene diphosphate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the mala...

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Bibliographische Detailangaben
Hauptverfasser: IIJIMA, Toru, UEDA, Naoko, XIA, Guangxin, XIE, Jianshu, JIA, Guohui, HAN, Jiansheng
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene diphosphate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene diphosphate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.